MK-1775 Inhibitor CAS No. 955365-80-7

Cat. No.	Name	Size	Price
KI1399	MK-1775	5 mg	$272
	MK-1775	10 mg	$432
	MK-1775	25 mg	$752
	MK-1775	50 mg	$1232

Chemical Characteristic

Product Name	MK-1775
CAS No.	955365-80-7
Molecular Weight	500.6
Formula	C₂₇H₃₂N₈O₂
Chemical Name	1-[6-(2-hydroxypropan-2-yl)pyridin-2-yl]-6-[4-(4-methylpiperazin-1-yl)anilino]-2-prop-2-enylpyrazolo[3,4-d]pyrimidin-3-one
Smiles	c1(nc2c(cn1)c(=O)n(n2c1cccc(n1)C(C)(C)O)CC=C)Nc1ccc(cc1)N1CCN(CC1)C
Chemical Structure

Biological activities

MK-1775 is a potent and selective small molecule inhibitor of Wee1 kinase with an IC50 of 5.2 nM. MK-1775 inhibits phosphorylation of CDC2 at Tyr15 (CDC2Y15) with an EC50 of 85 nM in cells pretreated with gemcitabine.^[1] MK-1775 abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines. ^[2] In vivo, MK-1775 potentiates the antitumor efficacies by gemcitabine, carboplatin, or cisplatin at tolerated doses. ^[1] MK-1775 enhances H1299 xenograft tumor response to fractionated radiotherapy. ^[2] MK-1775 selectively synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts. ^[3]

Protocols

In vitro: MK-1775 is dissolved in DMSO. ^[1]

References

[1] Hirai H, et al. Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Mol Cancer Ther. 2009, 8(11):2992-3000. [2] Bridges KA, et al. MK-1775, a novel Wee1 kinase inhibitor, radiosensitizes p53-defective human tumor cells. Clin Cancer Res. 2011, 17(17):5638-5648. [3] Rajeshkumar NV, et al. MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts. Clin Cancer Res. 2011, 17(9):2799-2806.

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